No effective therapy has yet developed for liver fibrosis/cirrhosis by directly inhibiting the accumulation of extracellular matrix. This study was undertaken to determine the effect of tetrandrine in rat model of liver fibrosis induced by carborn tetrachloride (CCl4) administration intraorally. Tetrandrine, a calcium channel blocker, is anti-inflammatory constituent of the families Menispermaceae and Ranunculaceae, which have been used as folk remedies in China. Repeated administration of CCl4 for 14 weeks to rats induced liver fibrosis with steatosis. Rats were killed after 4, 8 or 14 weeks of treatment with CCl4, CCl4 tetrandrine (30 mg/kg) or CCl4 tetrandrine (50 mg/kg). The histopathological findings of liver were observed semi-quantitatively by light microscopy and volume percentage of the collagen deposition was determined by image analyzer. Tetrandrine inhibited collagen deposition induced by CCl4 administration, as shown by less severe steatosis and fibrosis and significantly decreased volume percentage of collagen fibers in CCl4 tetrandrine treated animals compared with CCl4 only group. Thus, the administration of tetrandrine holds great promise for treating subjects with liver fibrosis/cirrhosis as a result of chronic hepatic injury.
Animals ; Calcium Channels ; Carbon Tetrachloride ; China ; Collagen ; Extracellular Matrix* ; Fibrosis* ; Humans ; Liver ; Liver Cirrhosis ; Medicine, Traditional ; Menispermaceae ; Microscopy ; Models, Animal ; Ranunculaceae ; Rats*

OBJECTIVETo study alkaloid constituents of Diploclisia affinis.

METHODThe air-dried vine stems of D. affinis were extracted with 90% EtOH three times at room temperature. The EtOH extract was suspended in H2 O and adjusted to pH 2 with 5% HCl solution. After extracted with petroleum ether and CHCl3 successively, the aqueous fraction was adjusted to pH 9 with 10% NH3 x H2O and extracted with CHCl3 again to afford the total alkaloids fraction. The compounds were isolated through column chromatography from the total alkaloids fraction. Their structures were determined on the basis of spectral analysis (MS, 1H-NMR, 13C-NMR).

RESULTFive alkaloids was identified as reticuline (1), asimilobine (2), acutumine (3), dihydroxyprotoberberine (4), stepholidine (5), were isolated from the vine stems of D. affinis.

CONCLUSIONAll the compounds were obtained from D. affinis for the first time.

Alkaloids ; chemistry ; Aporphines ; chemistry ; Benzylisoquinolines ; chemistry ; Berberine ; analogs & derivatives ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Ethanol ; chemistry ; Magnetic Resonance Spectroscopy ; Mass Spectrometry ; Menispermaceae ; chemistry ; Plant Stems ; chemistry ; Spiro Compounds ; chemistry

To study the chemical constituents from the rhizome of Menispermum dauricum,fifteen compounds,N-methylcorydaldine( 1),thalifoline( 2),stepholidine( 3),acutumine( 4),daurisoline( 5),acutumidine( 6),dauricicoline( 7),bianfugecine( 8),6-O-demethylmenisporphine( 9),bianfugedine( 10),dauricoside( 11),eleutheroside D( 12),aristolactone( 13),aristoloterpenateⅠ( 14) and aristolochic acid( 15) were isolated from 75% ethanol extract of Menispermi Rhizoma by using thin layer chromatography and column chromatography methods. Their structures were identified based on their physicochemical properties and spectral data. Among them,compounds 12-15 were obtained from the genus Menispermum for the first time. Six alkaloids with higher contents were subjected to evaluate the anti-hypoxic activities by using MTT method. As a result,six alkaloids exhibited significant anti-hypoxia activities.
Alkaloids ; Humans ; Hypoxia ; Menispermum ; Plant Extracts ; Rhizome

Tetrandrine (TET) and fangchinoline (FAN) are dominant bisbenzylisoquinoline (BBIQ) alkaloids from the roots of Stephania tetrandra of the family Menispermaceae. BBIQ alkaloids comprise two benzylisoquinoline units linked by oxygen bridges. The molecular structures of TET and FAN are exactly the same, except that TET has a methoxy (-OCH
Alkaloids/pharmacology* ; Benzylisoquinolines/pharmacology* ; Stephania tetrandra

Han stephania, also known as Stephania tetrandra, expelling wind, relieve pain and inducing diuresis for removing edema, is a traditional Chinese medicine for treating rheumatic arthralgia. Alkaloids have an important pharmacodynamic basis in S. tetrandra, and tetrandrine is one kind content of bisbenzylisoquinoline alkaloids, which has many biological activities. These activities include anti-tumor in many ways, clinically inhibiting multiple inflammatory factors, preventing and treating liver fibrosis and renal fibrosis and many other kinds of fibrotic diseases, and in addition, tetrandrine could work synergistically with other drugs. In recent years, through in-depth research by scholars at home and abroad, it has been found that tetrandrine has a protective effect on the nervous system and ischemia-reperfusion injury. At the same time, as a calcium ion antagonist, tetrandrine could effectively block the deposition of calcium ions inside and outside the cell. In summary, the application prospect of tetrandrine in clinical practice is very extensive. In this paper, the pharmacological effects of tetrandrine and the possible mechanisms for these effects are summarized, and review its current research progress. It is hoped that the possible application direction of tetrandrine can be revealed more comprehensively, and provide better enlightenment and ideas for clinical application.
Benzylisoquinolines/pharmacology* ; Drugs, Chinese Herbal/pharmacology* ; Humans ; Stephania tetrandra/chemistry*

OBJECTIVETo develop the system for the exclusive control substance of plant drug (CSPD) in traditional Chinese herbal medicines (TCHM), this paper investigated the (CSPD) of Radix Stephaniae Tetrandrae as well as its proton nuclear magnetic resonance (1H-NMR) and high performance liquid chromatography (HPLC) analytical methods for the purpose of original identification and quality control of the crude drug.

METHODThe CSPDs and their 1H-NMR and HPLC profiles of Radix Stephaniae Tetrandrae were obtained by standardized procedure. Chemical components were isolated from the CSPD by silica gel column chromatography. The assignments of the characteristic signals in 1H-NMR and HPLC profiles were achieved on the basis of elucidation of the isolates structures.

RESULTFor nine samples from the different sources in this paper, the 1H-NMR and HPLC profiles from eight sources had wonderful reproducibility and characteristics, and the other gave differences compared with the eight samples in the signal strength of the main components. Furthermore, seven compounds were isolated from CSPD and their chemical structures were authenticated by spectral analysis as tetrandrine, fangchinoline, tetrandrine-2'-N-beta-oxide, tetrandrine-2'-N-alpha-oxide, dicentrine, dicentrinone, and adenine, respectively. The 1H-NMR and HPLC profiles of the CSPD of Radix Stephaniae Tetrandrae showed mainly the characteristic signals of the bisbenzylisoquinoline alkaloids isolated in this work.

CONCLUSIONThe 1H-NMR and HPLC profiles of the CSPD of Radix Stephaniae Tetrandrae exhibit the structures and total composition of the main active constituents in it, and can be used for its original identification and quality evaluation.

Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; chemistry ; Magnetic Resonance Spectroscopy ; methods ; Quality Control ; Stephania tetrandra ; chemistry

OBJECTIVETo establish a new method for the determination of fangchinoline and tetrandrine in Stephania tetrandra and Fengtongan capsule by noanqueous capillary electrophoresis.

METHODSeparation was carried out in an uncoated fused capillary (50 cm x 75 microm i.d.) with a running buffer containing 50 mmol x L(-1) ammonium acetate, 1.0% acetic acid and 20% acetonitrile in methanol. A separation voltage of 20 kV and a UV detector wavelength at 214 nm were adopted. Sample was introduced from the anode.

RESULTThe calibration ranges were 1.00, 500 mg x L(-1) for both analytes. Under the optimum conditions, the relative standard deviation (RSD, n = 6) for the migration time of each analyte were 0.09%, 1.9% (intra-day) and 0.63%, 1.9% (inter-day); The RSD for the peak area of each analyte were 0.45%, 5.9% (intra-day) and 2.3%, 5.6% (inter-day), respectively. The contents of the analytes were determined easily with average recoveries 102% for fangchinoline and 105% for tetrandrine in S. tetrandra and 94.6% for fangchinoline and 98.7% for tetrandrine in Fengtongan capsules, respectively.

CONCLUSIONThe proposed method is simple, rapid, accurate and higher repeatable, and can be used to control of the quality of S. tetrandra and Fengtongan capsules.

Benzylisoquinolines ; analysis ; Calibration ; Capillary Electrochromatography ; methods ; Capsules ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; standards ; Plant Roots ; chemistry ; Plants, Medicinal ; chemistry ; Quality Control ; Reproducibility of Results ; Stephania tetrandra ; chemistry

AIMTo establish a method for separation and identification of alkaloids in Stephania tetrandra S. Moore methanol extracts by using non-aqueous capillary electrophoresis interfaced with electrospray ionization ion trap mass spectrometry.

METHODSThe molecular ions or adducts of alkaloids and fragments of specific parent ions were used for the identification. An uncoated capillary (86 cm x 75 microm ID, on-line UV detection occurred at 21 cm from the inlet of the capillary) was used. Ammonium acetate (50 mmol x L(-1)) containing 4% HAc in methanol was used as the running buffer; separation voltage was 25 kV. A coaxial sheath flow interface was used as the CE-MS interface; the electrospray voltage was 4.5 kV; the temperature of aluminium capillary was 170 degrees C; 60% isopropanol-39% water-1% HAc was used as the sheath liquid with the flow rate of 5 microL x min(-1); the collision energy of MS-MS was set at 30% and the least ion counts was 1 x 10(5).

RESULTS AND CONCLUSIONThe alkaloids in Stephania tetrandra S. Moore methanol extracts were separated and identified by CE-ESI-MS/MS. The proposed method is of high accuracy and can be used for the investigation of traditional Chinese medicine.

Alkaloids ; analysis ; isolation & purification ; Benzylisoquinolines ; analysis ; isolation & purification ; Electrophoresis, Capillary ; methods ; Plants, Medicinal ; chemistry ; Spectrometry, Mass, Electrospray Ionization ; methods ; Stephania tetrandra ; chemistry

Tinospora cordifolia (Guduchi or Gurjo), a herbaceous vine or climbing deciduous shrub, is consider as an important medicine in the Ayurvedic system of medication, which is available in India, China, Myanmar, Bangladesh and Srilanka. Menispermaceae is the family of this compound. T. cordifolia have a variety of properties to treat various ailments such as fevers, jaundice, diabetes, dysentery, urinary infections, and skin diseases. This compound has been subjected to many chemicals, pharmacological, pre-clinical, or clinical investigations and some new therapeutic potential effects have been indicated. This review aims to summarize the critical information concerning in areas of chemical constituents, chemical structure, and pharmacokinetic activities such as anti-diabetic, anticancer, immune-modulatory, antivirus (especially in silico study about COVID-19), antioxidant, antimicrobial, hepatoprotective and its effect on cardiovascular and neurological disorders as well as rheumatoid arthritis. This traditional herb needs more experimental study on the clinical, pre-clinical study, and clinical efficacy of these compounds for the prevention and treatment of COVID-19 and needs large-scale clinical studies to prove the clinical efficacy of this compound, especially in stress-related diseases and other neuronal disorders.
Humans ; Tinospora/chemistry* ; COVID-19 ; Plant Extracts/chemistry* ; Antioxidants/chemistry*

AIMTo observe the effect of phenolic alkaloids of Menispermum dauricum (PAMD) on thrombosis and platelet aggregation, and to explore its mechanism of action.

METHODSThrombosis was observed with arteriovenous shunt thrombus model in rat; platelet aggregation was determined by Born's method; ultrastructure of platelet was observed by transmission electron microscope; TXB2 or 6-keto-PGF1alpha levels were assessed by radioimmunoassay; and NO was determined by colorimetric method.

RESULTSPAMD dose-dependently inhibited experimental thrombus formation, platelet aggregation induced by ADP, AA and THR in vivo and ultrastructure changes stimulated by THR; PAMD increased the generation of 6-keto-PGF1alpha in thoracic aortae and NO level in plasma; and had no influence on TXB2 release (P > 0.05).

CONCLUSIONPAMD inhibited thrombosis and platelet aggregation, and its mechanism might be due to the increase of PGI2 and NO level.

6-Ketoprostaglandin F1 alpha ; metabolism ; Alkaloids ; administration & dosage ; isolation & purification ; pharmacology ; Animals ; Aorta, Thoracic ; metabolism ; Benzylisoquinolines ; administration & dosage ; isolation & purification ; pharmacology ; Blood Platelets ; ultrastructure ; Dose-Response Relationship, Drug ; Epoprostenol ; metabolism ; Male ; Menispermum ; chemistry ; Nitric Oxide ; blood ; Plants, Medicinal ; chemistry ; Platelet Aggregation ; drug effects ; Rabbits ; Rats ; Rats, Sprague-Dawley ; Rhizome ; chemistry ; Tetrahydroisoquinolines ; administration & dosage ; isolation & purification ; pharmacology ; Thrombosis ; metabolism ; Thromboxane B2 ; metabolism